Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/354)
  • Patent number: 9562030
    Abstract: The present invention provides a process for the synthesis of olopatadine. Further, the invention discloses a process that results in improved yield of the desired Z isomer.
    Type: Grant
    Filed: March 19, 2014
    Date of Patent: February 7, 2017
    Assignee: Council of Scientific and Industrial Research
    Inventors: Subhash Prataprao Chavan, Pradeep Bhaskarrao Lasonkar
  • Publication number: 20150148390
    Abstract: The present invention relates to glioblastoma inhibiting compounds, in particular gambogic acid amid and derivatives thereof for the treatment of glioblastoma. Moreover, methods for determining whether a treatment with the compounds of the invention is suitable for a patient are disclosed.
    Type: Application
    Filed: June 15, 2012
    Publication date: May 28, 2015
    Applicant: Life & Brain GmbH
    Inventors: Björn Scheffler, Martin Glas, Matthias Simon, Sabine Gogolok, Daniel Trageser, Roman Reinartz, Anja Wieland
  • Patent number: 9000195
    Abstract: Olopatadine can be obtained by means of a process comprising hydrolysis of a compound of general formula (II), wherein Y is OR1, wherein R1 is C1-C7 alkyl, C3-C7 cycloalkyl, aryl, arylalkyl, or heterocycle; or NR2R3, wherein R2 and R3, independently from each other, are C1-C7 alkyl, aryl, arylalkyl, or R2 and R3 together with the nitrogen atom to which they are bound form a heterocycle of 3 to 7 members, obtained by means of a process comprising reacting the corresponding ester or amide of 6,11-dihydro-11-oxodibenz[b,e]oxepin-2-acetic acid with a suitable Wittig reagent, in the presence of a base in a reaction medium comprising an organic solvent.
    Type: Grant
    Filed: July 14, 2009
    Date of Patent: April 7, 2015
    Assignee: Crystal Pharma, S.A.U.
    Inventors: Luis Octavio Silva Guisasola, Lydia Mateos Burón, Antonio Lorente Bonde-Larsen, Luis Gerardo Gutiérrez Fuentes
  • Patent number: 8980939
    Abstract: A process for the preparation of olopatadine hydrochloride starting from an advanced intermediate.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: March 17, 2015
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Andrea Castellin, Clark Ferrari, Marco Galvagni
  • Publication number: 20150065703
    Abstract: Disclosed are a new method for synthesizing 7-membered fused heterocycles and compounds synthesized by the new method. The method involves a dual activation strategy using an N-heterocyclic carbene catalyst as a first Lewis base and another second Lewis base. Compounds synthesized by the disclosed method may include new benzoxopinone compounds, as well as benzoxepane compounds and benzoazepinone compounds that optionally may be derived from the disclosed benzoxopinone compounds.
    Type: Application
    Filed: August 22, 2014
    Publication date: March 5, 2015
    Applicant: Northwestern University
    Inventors: Karl A. Scheidt, Javier Izquierdo Ferrer
  • Publication number: 20150031677
    Abstract: Monomeric and dimeric trioxane thioacetals and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
    Type: Application
    Filed: February 28, 2013
    Publication date: January 29, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Gary H. Posner, Alexander M. Jacobine, Rachel D. Slack, Jennifer R. Mazzone
  • Patent number: 8927594
    Abstract: The invention relates to compounds from the soft coral and the generation thereof. The invention also relates to the uses of the compounds from the soft coral in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2.
    Type: Grant
    Filed: March 15, 2011
    Date of Patent: January 6, 2015
    Assignees: National Sun Yat-Sen University, National Museum of Marine Biology & Aquarium
    Inventors: Jyh-Horng Sheu, Wei-Hsien Wang, Zhi-Hong Wen, Bo-Wei Chen, Ping-Jyun Sung
  • Patent number: 8871953
    Abstract: The present invention relates to a novel process for the preparation of olopatadine hydrochloride starting from an advanced intermediate.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: October 28, 2014
    Assignee: F.I.S. Fabbrica Italiana Sintetiei S.p.A.
    Inventors: Andrea Castellin, Clark Ferrari, Marco Galvagni
  • Publication number: 20140309437
    Abstract: Process for the preparation of intermediates that are useful in the synthesis of active pharmaceutical ingredients (API), in particular active in the central nervous system.
    Type: Application
    Filed: April 8, 2014
    Publication date: October 16, 2014
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Marco ARTICO, Emanuele ATTOLINO
  • Publication number: 20140221468
    Abstract: Store operated calcium channel modulating compounds, and methods for using the same, are provided. These compounds and methods find use in a variety of applications in which modulation of store operated calcium channels is desired.
    Type: Application
    Filed: December 9, 2011
    Publication date: August 7, 2014
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Chan Young Park, Amir M. Sadaghiani, Ricardo Ei Dolmetsch
  • Patent number: 8741889
    Abstract: The present invention provides a method for treating a patient having cancer comprising administering to the patient a therapeutically effective amount of compound (1), or a pharmaceutically acceptable salt thereof, having the formula: The present invention also provides a kit containing the above compound.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: June 3, 2014
    Assignee: Hoffmann-La Roche Inc
    Inventors: John Frederick Boylan, Leopoldo Ladores Luistro, Kathryn Elizabeth Packman
  • Publication number: 20140107060
    Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.
    Type: Application
    Filed: December 16, 2013
    Publication date: April 17, 2014
    Applicant: University of North Carolina at Wilmington
    Inventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
  • Publication number: 20140107351
    Abstract: Fullerene?CTV complexes, comprising fullerene?CTV hemicarceplexes, formed by various cyclotriveratrylene (CTV)-based molecular cages and various fullerene guests are disclosed. A method of direct isolating at least a fullerene from fullerene mixtures by using the above fullerene CTV hemicarceplexes but without using crystallization or HPLC is also disclosed.
    Type: Application
    Filed: October 17, 2012
    Publication date: April 17, 2014
    Applicant: NATIONAL TAIWAN UNIVERSITY
    Inventors: Sheng-Hsien Chiu, Ming-Jhe Li
  • Publication number: 20140107084
    Abstract: The invention relates to doxepin, pharmaceutically acceptable salts and prodrugs of doxepin; compositions containing the same, and the use of any of the aforementioned for the treatment of sleep disorders.
    Type: Application
    Filed: October 3, 2013
    Publication date: April 17, 2014
    Applicants: ProCom One, Inc., Somaxon Pharmaceuticals, Inc.
    Inventors: Philip Jochelson, Neil B. Kavey
  • Patent number: 8680111
    Abstract: The invention relates to compounds of formula (?) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: March 25, 2014
    Assignee: Pfizer Inc.
    Inventors: Simon Bailey, Benjamin Joseph Burke, Michael Raymond Collins, Jingrong Jean Cui, Judith Gail Deal, Robert Louis Hoffman, Qinhua Huang, Ted William Johnson, Robert Steven Kania, John Charles Kath, Phuong Thi Quy Le, Michele Ann McTigue, Cynthia Louise Palmer, Paul Francis Richardson, Neal William Sach
  • Publication number: 20140073604
    Abstract: Disclosed are compounds that are conjugates of ladder frame polyether compounds and biologically active compounds or research compounds, pharmaceutical formulations comprising the conjugates, and methods of transporting the conjugates across biological membranes.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 13, 2014
    Applicant: UNIVERSITY OF NORTH CAROLINA AT WILMINGTON
    Inventor: UNIVERSITY OF NORTH CAROLINA AT WILMINGTON
  • Publication number: 20140066408
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: January 14, 2013
    Publication date: March 6, 2014
    Applicant: REATA PHARMACEUTICALS, INC.
    Inventor: REATA PHARMACEUTICALS, INC.
  • Patent number: 8653285
    Abstract: An aminopropylidene derivative having excellent histamine receptor antagonistic action, a compound which is useful as a pharmaceutical composition, especially as an active ingredient, having alleviated side effects in the central nervous system is described. In the aminopropylidene derivative, R1 and R2, which may be identical or different, stand for a hydrogen, a substituted carbonyl, a substituted carbonylalkyl, and acrylic acid, excluding a case where both are hydrogen; R3 and R4, which may be identical or different, stand for hydrogen, an alkyl which may be substituted with phenyl, or the like; A stands for unsubstituted or an oxo; B stands for a carbon or an oxygen; one of X and Y stands for a carbon and the other stands for a sulfur, a broken line part stands for a single bond or a double bond, and a wavy line stands for cis-form and/or trans-form.
    Type: Grant
    Filed: July 31, 2009
    Date of Patent: February 18, 2014
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Kunihiko Higashiura, Takashi Ogino, Taizo Ito, Koji Kunimasu, Kazuhito Furukawa
  • Patent number: 8653280
    Abstract: The present invention is directed to novel compounds of formula (I) as well as to the process for their preparation. Novel compounds of formula (I) can be converted into asenapine through an efficient process. The invention also relates to novel intermediates used in this process and their use in the preparation of compounds of formula (I).
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: February 18, 2014
    Assignee: Laboratories Lesvi, S.L.
    Inventors: Pere Dalmases Barjoan, Juan Huguet Clotet, Jordi Peirats Masia
  • Publication number: 20140024704
    Abstract: A process for the preparation of olopatadine hydrochloride starting from an advanced intermediate.
    Type: Application
    Filed: July 12, 2013
    Publication date: January 23, 2014
    Inventors: Andrea Castellin, Clark Ferrari, Marco Galvagni
  • Patent number: 8629135
    Abstract: A class of compounds useful in pharmaceutical compositions and methods for treating or preventing cancer is described. The compounds' ability to inhibit RET kinase is quantified, i.e., their respective RET IC50 and EC50 values are described. One such compound, known as cyclobenzaprine and herein as SW-01, has been identified as RET-specific with an IC50 of 300 nM. SW-01 inhibits RET autophosphorylation and blocks the growth and transformation of thyroid cancer cell lines. It has been further tested in pancreatic cancer, breast cancer, and SCLC cell lines. The compounds show utility for inhibition of survival and proliferation of tumor cells.
    Type: Grant
    Filed: July 14, 2009
    Date of Patent: January 14, 2014
    Assignee: Queen's University at Kingston
    Inventors: Taranjit S. Gujral, Lois M. Mulligan, Vinay K. Singh
  • Publication number: 20130296413
    Abstract: Desmethyldoxepin, isomers of desmethyldoxepin, and pharmaceutically acceptable salts and prodrugs of desmethyldoxepin; compositions containing the same, and the use of any of the aforementioned for the treatment of sleep disorders.
    Type: Application
    Filed: July 2, 2013
    Publication date: November 7, 2013
    Inventors: Neil B. Kavey, Susan E. Dube
  • Patent number: 8541625
    Abstract: Cyclic alkynes (e.g., cyclooctynes such as dibenzocyclooctynes) can be photochemically generated from cyclopropenones as disclosed herein. The cyclic alkynes can be reacted (e.g., in situ) with materials having alkyne-reactive groups (e.g., azide groups in a “click” reaction). In preferred embodiments, the generation and reaction of the cyclic alkyne can proceed in the absence of a catalyst (e.g., Cu(I)). These reactions can be useful, for example, for the selective labeling of living cells that are metabolically modified with azido-containing surface monosaccharides, or for light-directed surface patterning.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: September 24, 2013
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: Vladimir V. Popik, Andrei A. Poloukhtine, Geert-Jan Boons, Margaretha Wolfert
  • Publication number: 20130225835
    Abstract: The present invention is directed to novel compounds of formula (I) as well as to the process for their preparation. Novel compounds of formula (I) can be converted into asenapine through an efficient process. The invention also relates to novel intermediates used in this process and their use in the preparation of compounds of formula (I).
    Type: Application
    Filed: July 29, 2011
    Publication date: August 29, 2013
    Applicant: LABORATORIOS LESVI, S.L.
    Inventors: Pere Dalmases Barjoan, Juan Huguet Clotet, Jordi Peirats Masia
  • Patent number: 8513299
    Abstract: Methods of preventing early awakenings, and improving sleep efficiency in hours 7 and 8 of a period of sleep, by administration of low doses of doxepin (e.g., 1-6 mg).
    Type: Grant
    Filed: May 18, 2007
    Date of Patent: August 20, 2013
    Assignees: Pernix Sleep, Inc., Procom One, Inc.
    Inventors: Roberta L. Rogowski, Susan E. Dubé, Philip Jochelson
  • Patent number: 8501803
    Abstract: The present invention relates to a field of pharmaceutical chemistry, more specifically, the present invention relates to a garcinia derivative Formula (I), its preparing method, and medicinal use. Wherein the definitions of R1 and R2 are disclosed in the specification of the present invention, and the derivative of the present invention is a structurally simplified analogue of the gambogic acid compound; wherein the gambogic acid compound possesses anti-cancer characteristics, and could be used for preparation of anti-tumor drugs.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: August 6, 2013
    Assignee: China Pharmaceutical University
    Inventors: Qidong You, Xiaojian Wang, Qian Yang, Na Lu, Changjun Lin, Qinglong Guo
  • Patent number: 8486980
    Abstract: Provided is a tricyclic compound having a PPAR ? agonist activity, which is represented by the general formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:
    Type: Grant
    Filed: August 6, 2009
    Date of Patent: July 16, 2013
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Arata Yanagisawa, Keiji Uehara, Masahiro Matsubara, Kimihisa Ueno, Michihiko Suzuki, Takeshi Kuboyama, Keisuke Yamamoto, Tomohiro Tamura
  • Publication number: 20130164803
    Abstract: Cyclic alkynes (e.g., cyclooctynes such as dibenzocyclooctynes) can be photochemically generated from cyclopropenones as disclosed herein. The cyclic alkynes can be reacted (e.g., in situ) with materials having alkyne-reactive groups (e.g., azide groups in a “click” reaction). In preferred embodiments, the generation and reaction of the cyclic alkyne can proceed in the absence of a catalyst (e.g., Cu(I)). These reactions can be useful, for example, for the selective labeling of living cells that are metabolically modified with azido-containing surface monosaccharides, or for light-directed surface patterning.
    Type: Application
    Filed: August 6, 2012
    Publication date: June 27, 2013
    Applicant: University of George Research Foundation, Inc.
    Inventors: VLADIMIR V. POPIK, Andrei A. Poloukhtine, Geert-Jan Boons, Margaretha Wolfert
  • Publication number: 20130123235
    Abstract: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Application
    Filed: July 21, 2011
    Publication date: May 16, 2013
    Inventors: David Clark, Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler
  • Patent number: 8440820
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: May 14, 2013
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
  • Patent number: 8399690
    Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: March 19, 2013
    Assignees: Genentech, Inc., F. Hoffman-La Roche Inc.
    Inventors: Steven Do, Richard Goldsmith, Tim Heffron, Aleksandr Kolesnikov, Steven Staben, Alan G. Olivero, Michael Siu, Daniel P. Sutherlin, Bing-Yan Zhu, Paul Goldsmith, Tracy Bayliss, Adrian Folkes, Neil Pegg
  • Publication number: 20130022669
    Abstract: The present invention relates to branched polyethyleneglycol (PEG) derivatives consisting of a molecule with a quaternary carbon connected to three PEG chains, wherein all three PEG chains are of equal length and each comprises 1-30 —OCH2CH2— units, and one group with at least one carbon atom, wherein said at least one carbon atom is attached to the quaternary carbon. Also compositions containing such derivatives and use of such derivatives are disclosed.
    Type: Application
    Filed: March 29, 2011
    Publication date: January 24, 2013
    Applicant: SPAGO IMAGING AB
    Inventors: Oskar Axelsson, Fredrik Ek
  • Publication number: 20120295318
    Abstract: Cyclic alkynes (e.g., cyclooctynes such as dibenzocyclooctynes) can be photochemically generated from cyclopropenones as disclosed herein. The cyclic alkynes can be reacted (e.g., in situ) with materials having alkyne-reactive groups (e.g., azide groups in a “click” reaction). In preferred embodiments, the generation and reaction of the cyclic alkyne can proceed in the absence of a catalyst (e.g., Cu(I)). These reactions can be useful, for example, for the selective labeling of living cells that are metabolically modified with azido-containing surface monosaccharides, or for light-directed surface patterning.
    Type: Application
    Filed: August 6, 2012
    Publication date: November 22, 2012
    Applicant: University of George Research Foundation, Inc.
    Inventors: VLADIMIR V. POPIK, Andrei A. Poloukhtine, Geert-Jan Boons, Margaretha Wolfert
  • Publication number: 20120283321
    Abstract: The present invention relates to the use of a compound with the following chemical structure: for the preparation of a medicament, preferably designed for the prevention or treatment of pathological processes related to the tau and ?-amyloid proteins. Preferably, the compound used is gambierol.
    Type: Application
    Filed: September 29, 2010
    Publication date: November 8, 2012
    Applicant: Universidade De Santiago De Compostela
    Inventors: Luis Miguel Botana López, Eva Alonso López, Carmen Vale González
  • Publication number: 20120245223
    Abstract: The present invention refers to the use of a compound with the chemical structure for the preparation of a medicinal drug, preferably for the prevention or the treatment of pathological processes related to the tau and ?-amyloid proteins. The compound preferably used is gymnodimine.
    Type: Application
    Filed: September 2, 2010
    Publication date: September 27, 2012
    Applicant: UNIVERSIDADE DE SANTIAGE DE COMPOSTELA
    Inventors: Luis Miguel Botana López, Eva Alonso López, Carmen Vale González
  • Patent number: 8236850
    Abstract: The present invention relates to dimeric derivatives of 10-trifluoromethylated artemisinin of formula (I): or a pharmaceutically acceptable salt thereof with B1 and B2 selected from C?O, CHOH and CH2, as well as to their use in treating cancer and to their preparation method.
    Type: Grant
    Filed: December 22, 2008
    Date of Patent: August 7, 2012
    Assignees: Pierre Fabre Medicament, Centre National de la Recherche Scientifique, Universite Paris-Sud 11
    Inventors: Jean-Pierre Begue, Danielle Bonnet-Delpon, Benoît Crousse, Fabienne Grellepois, Constance Chollet, Jacques Fahy, Céline Mordant
  • Patent number: 8232417
    Abstract: The present invention discloses certain derivatives of artemisinin and the active principles contained in Artemisia annua extracts with amino acids, peptides, and amino sugars and salts thereof (formula I).
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: July 31, 2012
    Assignee: Bioderm Research
    Inventor: Shyam K Gupta
  • Patent number: 8193376
    Abstract: The present invention discloses certain derivatives of artemisinin and the active principles contained in Artemisia annua extracts with amino acids, peptides, and amino sugars, and isomers and salts thereof (formula I).
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: June 5, 2012
    Assignee: Bioderm Research
    Inventor: Shyam K Gupta
  • Publication number: 20120122810
    Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.
    Type: Application
    Filed: January 23, 2012
    Publication date: May 17, 2012
    Inventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
  • Patent number: 8178578
    Abstract: A compound of formula (I) is described; wherein the substituents are as defined in the text and wherein the compound is intended for use in the production of a vascular damaging effect in a warm-blooded animal.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: May 15, 2012
    Assignee: The University of Manchester
    Inventors: Timothy William Wallace, David John Edwards, John Anthony Hadfield
  • Publication number: 20120115862
    Abstract: The present invention relates to compounds of the formula I wherein R1, R2, R3, R4, X and Y have the meanings given in the description. The compounds have an action which is immunomodulating and inhibits or regulates the release of IL-1? and/or TNF-?. They can therefore be used for treatment of diseases connected with a disturbance in the immune system.
    Type: Application
    Filed: October 9, 2009
    Publication date: May 10, 2012
    Inventors: Stefan Laufer, Wolfgang Albrecht
  • Publication number: 20120095217
    Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.
    Type: Application
    Filed: January 8, 2010
    Publication date: April 19, 2012
    Inventors: Tobias Ritter, Laura Brass, Curtis Keith, Alan Watson, David J. Greenblatt
  • Publication number: 20120095184
    Abstract: A monomer having the general formula: in which R1 is any substitution; R2 is any substitution; R1 and R2 may be linked to form a saturated or unsaturated ring; L represents a reactive leaving group; X and Y each independently represent CR2, O, BR, NR, SiR2, S, S?O, SO2, PR or P?O(R) wherein R in each occurrence is independently selected from H or a substituent; Z represents a single bond or a divalent atom or group, wherein X—Z—Y forms an unconjugated ring or chain, with the proviso that at least one of R1 and R2 is an aryl or heteroaryl group if Z is a single bond.
    Type: Application
    Filed: April 15, 2010
    Publication date: April 19, 2012
    Applicants: Sumitomo Chemical Company Limited, Cambridge Display Technology Limited
    Inventors: Mary McKiernan, Johathan Pillow
  • Publication number: 20120077778
    Abstract: Disclosed are compounds that are conjugates of ladder frame polyether compounds and biologically active compounds or research compounds, pharmaceutical formulations comprising the conjugates, and methods of transporting the conjugates across biological membranes.
    Type: Application
    Filed: September 29, 2010
    Publication date: March 29, 2012
    Inventors: Andrea Bourdelais, Daniel Baden, Allan Goodman, Steven Fontana
  • Publication number: 20120071547
    Abstract: The invention relates to compounds from the soft coral and the generation thereof. The invention also relates to the uses of the compounds from the soft coral in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2.
    Type: Application
    Filed: March 15, 2011
    Publication date: March 22, 2012
    Applicants: NATIONAL MUSEUM OF MARINE BIOLOGY & AQUARIUM, NATIONAL SUN YAT-SEN UNIVERSITY
    Inventors: JYH-HORNG SHEU, WEI-HSIEN WANG, ZHI-HONG WEN, BO-WEI CHEN, PING-JYUN SUNG
  • Publication number: 20120059050
    Abstract: The present invention relates to a field of pharmaceutical chemistry, more specifically, the present invention relates to a garcinia derivative Formula (I), its preparing method, and medicinal use. Wherein the definitions of R1 and R2 are disclosed in the specification of the present invention, and the derivative of the present invention is a structurally simplified analogue of the gambogic acid compound; wherein the gambogic acid compound possesses anti-cancer characteristics, and could be used for preparation of anti-tumor drugs.
    Type: Application
    Filed: November 9, 2010
    Publication date: March 8, 2012
    Inventors: Qidong You, Xiaojian Wang, Qian Yang, Na Lu, Changjun Lin, Qinglong Guo
  • Publication number: 20120035170
    Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.
    Type: Application
    Filed: August 22, 2011
    Publication date: February 9, 2012
    Inventors: José Maria Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
  • Publication number: 20120016138
    Abstract: The present invention relates to a process for the preparation of olopatadine and, more particularly, to an improved method of synthesizing olopatadine which comprises reacting a dibenz[b,e]oxepin-11-one derivative of formula (III) and a suitable reagent under Witting condition, and to the intermediate 11-[(Z)-3-(dimethylamino)-propylidene]-6-11-dihydrodibenz[b,e]-oxepin-2-acet-amide p-toluensulfonate salt.
    Type: Application
    Filed: February 1, 2010
    Publication date: January 19, 2012
    Applicant: ZACH SYSTEM S.P.A.
    Inventors: Alberto Guidi, Filippo Chiarello, Gianmauro Orru', Massimo Verzini, Livius Cotarca, Jean-Claude Kizirian, Elisenda Trepat Guixer, Francisco Marquillas Olondriz
  • Patent number: RE45288
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: December 9, 2014
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
  • Patent number: RE45325
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: January 6, 2015
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick